Assay Detail
Binding
CHEMBL1049546
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Displacement of [3H]TO901317 from human recombinant LXRalpha expressed in Escherichia coli by flashplate method
20
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Quinoline-3-carboxamide containing sulfones as liver X receptor (LXR) agonists with binding selectivity for LXRbeta and low blood-brain penetration.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 20 | 6.26 | 8.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL595689 | — | — | 1 | 8.70 |
| CHEMBL590098 | — | — | 1 | 8.18 |
| CHEMBL62136 | T091317 | — | 1 | 7.89 |
| CHEMBL600244 | — | — | 1 | 7.87 |
| CHEMBL593739 | — | — | 1 | 6.54 |
| CHEMBL590584 | — | — | 1 | 6.35 |
| CHEMBL589613 | — | — | 1 | 6.34 |
| CHEMBL590828 | — | — | 1 | 6.26 |
| CHEMBL593267 | — | — | 1 | 6.26 |
| CHEMBL591582 | — | — | 1 | 6.22 |
| CHEMBL604259 | — | — | 1 | 6.12 |
| CHEMBL606139 | — | — | 1 | 5.87 |
| CHEMBL602446 | — | — | 1 | 5.75 |
| CHEMBL590350 | — | — | 1 | 5.20 |
| CHEMBL600851 | — | — | 1 | 5.16 |
| CHEMBL593740 | — | — | 1 | 4.90 |
| CHEMBL590351 | — | — | 1 | 4.58 |
| CHEMBL590586 | — | — | 1 | 4.53 |
| CHEMBL591815 | — | — | 1 | - |
| CHEMBL606862 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL595689 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL590098 | — | IC50 | = | 6.6 | nM | 8.18 |
| CHEMBL62136 | T091317 | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL600244 | — | IC50 | = | 13.4 | nM | 7.87 |
| CHEMBL593739 | — | IC50 | = | 286.0 | nM | 6.54 |
| CHEMBL590584 | — | IC50 | = | 445.0 | nM | 6.35 |
| CHEMBL589613 | — | IC50 | = | 453.0 | nM | 6.34 |
| CHEMBL590828 | — | IC50 | = | 552.0 | nM | 6.26 |
| CHEMBL593267 | — | IC50 | = | 543.0 | nM | 6.26 |
| CHEMBL591582 | — | IC50 | = | 600.0 | nM | 6.22 |
| CHEMBL604259 | — | IC50 | = | 756.0 | nM | 6.12 |
| CHEMBL606139 | — | IC50 | = | 1365.0 | nM | 5.87 |
| CHEMBL602446 | — | IC50 | = | 1772.0 | nM | 5.75 |
| CHEMBL590350 | — | IC50 | = | 6348.0 | nM | 5.20 |
| CHEMBL600851 | — | IC50 | = | 6864.0 | nM | 5.16 |
| CHEMBL593740 | — | IC50 | = | 12700.0 | nM | 4.90 |
| CHEMBL590351 | — | IC50 | = | 26613.0 | nM | 4.58 |
| CHEMBL590586 | — | IC50 | = | 29850.0 | nM | 4.53 |
| CHEMBL591815 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL606862 | — | IC50 | > | 10000.0 | nM | - |